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1. 发明公开

EP3337488A1 TREATMENT AND PREVENTION OF NEISSERIA GONORRHOEAE INFECTION USING CMP-ACTIVATED NONULOSONATE ANALOG COMPOUNDS 审中-实审
公开(公告)号：EP3337488A1
公开(公告)日：2018-06-27
申请号：EP16836327.3
申请日：2016-08-19
申请人： National Research Council of Canada
发明人： SCHOENHOFEN, Ian C.
IPC分类号： A61K31/7068 , A61K31/7012 , A61K9/00 , A61P31/04 , C07H19/01 , C07H7/02
CPC分类号： A61K31/7012 , A61K9/0034 , A61K31/7068 , A61K45/06 , A61K2300/00
摘要： There is provided a method for treating or preventing a Neisseria gonorrhoeae infection in a subject, comprising administering to the subject an effective amount of a compound of general formula I below or a pharmaceutical composition comprising said compound, or a derivative thereof, or a pharmaceutically acceptable salt thereof, or a solvate or hydrate thereof, or a stereoisomer thereof.

2. 发明公开

EP3170834A1 CRYSTALLINE FORMS OF (1S,3'R,4'S,5'S,6'R)-6-[(4-ETHYLPHENYL)METHYL]-3',4',5',6'-TETRAHYDRO-6'- (HYDROXYMETHYL)SPIRO[ISOBENZOFURAN-1(3H) 2'-[2H]PYRAN]-3',4',5'-TRIOL 有权
标题翻译：（1S，3'R，4'S，5'S，6'R）-6 - [（4-乙基苯基）甲基] -3'，4'，5'，6'-四氢-6' - （羟基甲基） SPIRO [异苯并呋喃-1（3H）2' - [2H]吡喃] -3'，4'，5'-三醇
公开(公告)号：EP3170834A1
公开(公告)日：2017-05-24
申请号：EP16202285.9
申请日：2009-06-19
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： MURAKATA, Masatoshi , IKEDA, Takuma , KIMURA, Nobuaki , KAWASE, Akira , NAGASE, Masahiro
IPC分类号： C07H19/01 , C07H1/00 , C07D493/10
CPC分类号： C07H19/01 , C07D493/10 , C07H1/00 , C07H7/04 , C07H13/04 , C07H23/00
摘要： The present invention relates to crystalline forms of the compound represented by Formula (XI), which is useful for preventing or treating diabetes.
摘要翻译：本发明涉及由式（XI）表示的化合物的结晶形式，其可用于预防或治疗糖尿病。

3. 发明公开

EP2821495A4 HIGH-PURITY ACID-FORM SOPHOROLIPID (SL) CONTAINING COMPOSITION AND PROCESS FOR PREPARING SAME 有权
标题翻译：取高纯度槐糖脂（SL）以酸的形式和方法及其生产成分
公开(公告)号：EP2821495A4
公开(公告)日：2015-10-21
申请号：EP13755243
申请日：2013-03-01
申请人： SARAYA CO LTD
发明人： HIRATA YOSHIHIKO , RYU MIZUYUKI , ITO HITOSHI , ARAKI MICHIAKI
IPC分类号： C12P19/12 , A23L1/30 , A61K8/73 , A61Q19/00 , B01F17/56 , C07H15/04 , C07H19/01
CPC分类号： C07H15/10 , A23L29/10 , A23L33/12 , A61K8/602 , A61K2800/10 , A61Q19/00
摘要： The present invention provides a high-purity acid-form sophorolipid (SL)-containing composition characterized by substantially not containing acetic acid. The high-purity acid-form SL-containing composition can be produced, for example, by the following method: (i) adjusting the pH of a partially purified acid-form SL-containing composition to an acidic range; and (ii-a) subjecting an acidified partially purified acid-form SL-containing composition obtained in step (i) to chromatography to acquire a fraction containing an acid-form SL, or (ii-b) leaving the acidified partially purified acid-form SL-containing composition obtained in step (i) to stand under a low-temperature condition to acquire a resulting gelled object.

4. 发明授权

EP1802635B8 Heteroatoms-containing tricyclic compounds 有权转让
标题翻译：含有杂原子的三环化合物
公开(公告)号：EP1802635B8
公开(公告)日：2013-04-17
申请号：EP05793907.6
申请日：2005-10-10
申请人： MEDA Pharma S.à.r.l.
发明人： GRASSBERGER, Maximilian , HORVATH, Amarylla
IPC分类号： C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01 , Y02P20/55

5. 发明公开

EP2048153A4 SUBSTITUTED SPIROKETAL DERIVATIVE AND USE THEREOF AS DRUG FOR TREATING DIABETES 审中-公开
标题翻译：取代SPIROKETALDERIVAT和其作为药物治疗糖尿病
公开(公告)号：EP2048153A4
公开(公告)日：2013-01-23
申请号：EP07791500
申请日：2007-07-27
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： SATO TSUTOMU , HONDA KIYOFUMI , KAWAI TAKAHIRO , AHN KOO HYEON
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07H19/01

6. 发明公开

EP2048152A1 FUSED RING SPIROKETAL DERIVATIVE AND USE THEREOF AS DRUG FOR TREATING DIABETES 审中-公开
标题翻译： SPIROKETALDERIVATE稠环和其作为药物治疗糖尿病
公开(公告)号：EP2048152A1
公开(公告)日：2009-04-15
申请号：EP07791496.8
申请日：2007-07-27
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： SATO, Tsutomu , OHTAKE, Yoshihito , NISHIMOTO, Masahiro , EMURA, Takashi , KOBAYASHI, Takamitsu , YAMAGUCHI, Marina , TAKAMI, Kyouko
IPC分类号： C07H19/01 , A61K31/7048 , A61K31/7056 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07H19/01
摘要： Provided are a compound represented by Formula (I):

wherein R 1 , R 2 , R 3 , and R 4 are each independently selected from a hydrogen atom, a C 1-6 alkyl group which may be substituted, a C 7-14 aralkyl group which may be substituted and -C(=O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f).

, or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供由式（I）表示的化合物：其中R 1，R 2，R 3，和R 4各自独立地选自氢原子，可被取代的C 1-6烷基团，一个C 7-14 可被取代的芳烷基和基团-C（= O）的Rx; n表示选自1和2选择的整数; 和环Ar为从由下式（A）至（f）表示的基团。或其前药或其药学上可接受的盐以及药物制剂和含有寻求的化合物或其前药的药物组合物，或其药学上可接受的盐。

7. 发明授权

EP1421094B1 4"-DEOXY-4"-(S)-AMINO AVERMECTIN DERIVATIVES 有权
标题翻译： 4 '' - 脱氧-4 '' - （S） - 氨基阿维菌素衍生物
公开(公告)号：EP1421094B1
公开(公告)日：2008-10-15
申请号：EP02767411.8
申请日：2002-08-20
申请人： Merial Limited
发明人： TOBLER, Hans
IPC分类号： C07H19/01 , A01N43/90
CPC分类号： C07H19/01 , A01N43/90
摘要： A description is given of compounds of the formula which in the 4"-position has the (S-)configuration and wherein R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is hydrogen, optionally substituted C1-C12alkyl or optionally substituted C2-C12alkenyl; R3 is C1-C12alkyl, optionally substituted C1-C12alkyl, optionally substituted C1-C12alkoxy-C1-C12alkyl,optionally substituted C3-C12cycloalkyl, optionally substituted C2-C12alkenyl; optionally substituted C4-C12cycloalkenyl,optionally substituted C2-C12alkynyl; or R2 and R3 together are a three- to seven-membered alkylene or four- to seven-membered alkenylene bridge in each of which a CH2 group may have been replaced by O, S or NR4; X is O or S; R4 is C1-C8alkyl, C3-C8cycloalkyl, C2-C8alkenyl, C2-C8alkynyl, benzyl or C(=O)-R5; R5 is for example H, OH, SH, C1-C12alkyl, C2-C8alkenyl, C2-C8alkynylyl or C1-C12haloalkyl; and, where appropriate, E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form; to a process for the preparation of, and to the use of, such compounds and isomers and tautomers thereof; to starting compounds for the preparation of compounds of formula (I); to pesticidal compositions in which the active ingredient has been selected from the compounds of formula (I) and tautomers thereof; and to a method of controlling pests using such compositions.

8. 发明公开

EP1852439A1 SPIROKETAL DERIVATIVE AND USE THEREOF AS DIABETIC MEDICINE 有权
标题翻译： SPIROKETAL-DERIVAT UND DESSEN VERWENDUNG ALS DIABETES-HEILMITTEL
公开(公告)号：EP1852439A1
公开(公告)日：2007-11-07
申请号：EP06712450.3
申请日：2006-01-27
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： KOBAYASHI, Takamitsu , SATO, Tsutomu , NISHIMOTO, Masahiro
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07D311/96 , C07D491/153 , C07D493/10 , C07H19/01
摘要： The present invention provides a compound of Formula (I):

wherein R 1 , R 2 , R 3 and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and -C(=O)Rx; Rx represents an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents -(CH 2 ) m -(L) p - or -(L)p-(CH 2 ) m -; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents -O-, -S- or -NR 5 -; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.
摘要翻译：本发明提供式（I）的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，任选取代的C 1 -C 6烷基，任选取代的C 7 - C 14芳烷基和-C（= O）Rx; Rx表示任选取代的C 1 -C 6烷基，任选取代的芳基，任选取代的杂芳基，任选取代的C 1 -C 6烷氧基或-NReRf; Ar 1表示任选取代的芳族碳环或任选单取代的芳族杂环; Q表示 - （CH 2）m - （L）p - 或 - （L）p-（CH 2）m - ; m表示选自0至2的整数，n表示选自1和2的整数，p表示选自0和1的整数; L表示-O - ， - S-或-NR 5 - ; A表示任选取代的芳基或任选取代的杂芳基，其前药及其药学上可接受的盐以及包含这种化合物的药物组合物或药物组合物。

9. 发明公开

EP1817317A1 METHODS FOR PREPARING PIMECROLIMUS 有权
标题翻译：用于生产吡美莫司
公开(公告)号：EP1817317A1
公开(公告)日：2007-08-15
申请号：EP05848723.2
申请日：2005-12-01
申请人： Teva Gyógyszergyár Zártköruen Muködo Részvenytarsaság
发明人： GYOLLAI, Viktor , SZABO, Csaba
IPC分类号： C07D498/18 , C07H19/01 , A61K31/395 , A61K31/70 , A61P17/00
CPC分类号： C07D498/18 , A61K9/145 , A61K9/1688 , A61K31/4745 , C07D491/14 , C07H19/01
摘要： The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.

10. 发明公开

EP1497283A4 MALEIC ACID SALT OF(2S)-N-(5(AMINO(IMINO)METHYL)-2-THIENYL)METHYL-1-(2R)-2-((2R)-2-((CARBOXYMETHYL)AMINO)3,3-DIPHENYLPROPANOYL)-2-PYRROLIDINE CARBOXAMIDE AND A PROCESS FOR 审中-公开
标题翻译：（2S）-N-（5-氨基（亚氨基）甲基] -2-噻吩甲酰基-1 - （（2R）-2-（羧甲基）氨基] -3,3-二苯基丙酰基] -2-吡咯烷碳酰胺氨基甲酸酯
公开(公告)号：EP1497283A4
公开(公告)日：2006-01-11
申请号：EP03744724
申请日：2003-03-21
申请人： LG LIFE SCIENCES LTD
发明人： KIM AERI , PARK JAE-HYEON , YOON SUK-KYOON , PARK CHEOL-WON , CHO KWAN-HYUNG
IPC分类号： A61K38/00 , A61P7/02 , C07C51/41 , C07D409/12 , C07K1/30 , C07K5/065 , C07C57/30 , C07D205/04 , C07D207/16 , C07H19/01 , C07K5/06
CPC分类号： C07K5/06078 , C07K2299/00
摘要： The present invention relates to a maleic acid salt of (2S)-N-{5-[amino(imino)methyl]-2-thienyl}methyl-1-{(2R)-2-[(carboxymethyl)amino]-3,3-diphenylpropanoyl}-2-pyrrolidinecarboxamide.
摘要翻译：本发明涉及（2S）-N- {5- [氨基（亚氨基）甲基] -2-噻吩基}甲基-1 - {（2R）-2 - [（羧甲基）氨基] -3 ，3- diphenylpropanoyl} -2-吡咯烷甲酰胺。

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